Nonsugarbase compounded tablet or lozenge base material for use in the preparation of suckable,structurally sound and hard at room temperature,nonhygroscopic,noncariesforming tablets or lozenges



United States Patent 3,525,791 NONSUGARBASE COMPOUNDED TABLET 0R LOZENGE BASE MATERIAL FOR USE IN THE PREPARATION OF SUCKABLE, STRUCTUR- ALLY SOUND AND HARD AT ROOM TEMPER- ATURE, NONHYGROSCOPIC, NGNCARIES- FORMING TABLETS 0R LOZENGES Gerhard W. Ahrens, 1781 E. th St., New York, NY. 11229 No Drawing. Filed May 20, 1968, Ser. No. 730,626 Int. Cl. A61k 15/00 US. Cl, 424-280 2 Claims ABSTRACT OF THE DISCLOSURE Sugarfree, suckable, structurally sound and hard at room temperature, nonhygroscopic, noncariesforming tablets or lozenges possessing maximum stability and shelf life are prepared using a new nonsugarbase compounded tablet or lozenge base material possessing medical properties of its own, which is nonhygroscopic, cold water insoluble, edible, palatable, structurally sound and hard at room temperature and dispersible and/or dissolvable in mouth fluids through sucking action for the release of the said medical properties of its own and of the properties of any other desired and suitable ingredients that may have been incorporated in the said tablets or lozenges prepared therewith.

This compounded homogeneously textured, nonsugarbase, nonhygroscopic, cold water insoluble, edible, palatable, structurally sound and hard at room temperature and dispersible and/ or dissolvable in mouth fluids by sucking action tablet or lozenge base material as described herein is formed by the incorporation in the heretofore thought of being unsuitable because of its structural softness and weakness at room temperature but edible, palatable, nonhygroscopic and cold water insoluble solid fatty acid mono-ester of sorbitan sorbitan mono-stearate and compounding therewith of sufiicient amounts of the organic acid metal salt possessing medical properties calcium ascorbate dihydrate which is a nonhygroscopic and hard crystallinic but watersoluble material, alone, or in conjunction with a partial substituent for the same selected from a group of anti-caries and caries-preventive phos phate salts also capable of acting as mineral balancing agent for calcium metabolically such as dibasic magnesium phosphate, whereby the medical properties of both the calcium ascorbate dihydrate" and the dibasic magnesium phosphate are transferred to the resulting said new tablet or lozenge base material.

This invention relates to sugar-free, suokable, structurally sound and hard at room temperature, nonhygroscopic, noncariesforming tablets or lozenges possesing maximum stability and shelf life prepared by the use of a new nonsugarbase, compounded tablet or lozenge base material possessing medical properties of its own, which is nonhygroscopic, cold water insoluble, edible, palatable, structurally sound and hard at room temperature and dispersible and/ or dissolvable in mouth fluids through sucking action to cause the release thereby not only of the medical properties of its own but also of the properties of any other suitable ingredients that may have been incorporated in the said tablets or lozenges prepared therewith.

Known edible and palatable tablet or lozenge base materials heretofore employed in the preparation of tablets or lozenges did not only not possess medical properties of its own but the great majority thereof were sugarbased materials with medical agents simply added thereto and/or incorporated therein to provide for medical rop erties in these tablets or lozenges prepared therewith. However, these sugar-based materials, although hitherto thought of to be the only such tablet or lozenge base materials capable of providing the desired and necessary structural hardness and soundness at room temperature for the tablets or lozenges prepared therewith, lacked in the essential property of nonhygroscopicity which is so importantly necessary for the attainment of maximum stability and shelf life in tablets or lozenges, particularly in those containing medical agents, vitamins and the like of a more or less perishable nature and which therefor had quite often additionally to be provided with protective coatings in the attempt, at least partially, to overcome the drawbacks of hygroscopicity and extend the stability and shelf life of such tablets or lozenges accordingly. Too, sugar-based tablet or lozenge base materials conferred to tablets or lozenges prepared therewith cariesproneness and presented a threat to diabetics in particular.

Nonsugarbase tablet or lozenge base materials have been proposed in the past to replace, at least in part, sugar-based tablets or lozenge base materials, such as, for instance by gum-based; -carbohydrate-based; -watersoluble cellulose-ester-based; pectin-based; -protein-based and even solid polyethyleneglycol-based materials, the

latter despite of its wellknown and recognized health hazard to humans (Mercks Index, 7th Edition, 1960, p. 213 and p. 429). All these materials, however although possessing water-solubility as needed, failed to possess either some medical properties of its own or the important property of nonhygroscopicity so essentially necessary for the attainment of maximum stability and shelf life in tablets or lozenges and especially and particularly in such containing medical agents. Too, neither of the above nonsugarbase materials was able to confer to tablets or lozenges the so necessarily desired structural soundness and hardness at room temperature as to be, at least partially, comparable with sugar-based materials, so that, since there appeared to exist a rather definite structural disadvantage in replacing sugar-based materials with any heretofore known non-sugarbase materials and since also the protection costs and material costs of any known nonsurgarbase materials is higher than the production and material costs of sugar-based materials and no other advantage except sugarlessness could be gained sugarbased materials continued and continue to be used in the preparation of the overwhelming majority of tablets or lozenges, with or without added medical agents, and thus continued to pose not only a major health hazard to diabetics or to diabetics-to-be but also to the maintenance of general tooth health, as such sugar-based tablets or lozenges are cariesforming as well as do present, according to published authoritative data, prime factors in the development of rampant caries formations, clearly thereby indicating that there exists presently an obvious and urgent need for the development of an improved nonsugarbase tablet or lozenge base material which is able to provide tablets or lozenges that are su'garfree, structurally sound and hard at room temperature, nonhygroscopic for the attainment of maximum stability and shelf life for said tablets or lozenges and, in addition, also capable to confer upon the same noncariesforming and own medical properties in addition to properties possessed therein as result of other ingredients incorporated in said tablets or lozenges during manufacturing.

With the event of my invention, however, this urgent need for an improved nonsugarbase tablet or lozenge material which is able to provide tablets or lozenges that are sugarfree, structurally sound and hard at room temperature, nonhygroscopic for the attainment of maximum stability and shelflife for said tablets or lozenges and which, in addition, also confers upon said tablets or lozenges noncariesforming and medical properties of its own in addition to properties possessed therein as result of other ingredients incorporated therein during the manufacture thereof, has been fully fulfilled and a new nonsugarbase compounded tablet or lozenge base material possessing medical properties of its own been provided which is nonhygroscopic, cold-Water insoluble, edible and palatable, structurally sound and hard at room temperature and dispersible and/or dissolvable in mouth fluids through sucking action for the release thereby of said medical properties of its own and the properties of any other ingredients that might have been incorporated in tablets or lozenges prepared by the use of said new nonsugarbase compounded tablet or lozenge base material of the invention. Thus, the new nonsugarbase compounded tablet or lozenge base material of the invention is. not only providing a new material but also one which is eminently suitable for its purpose on account of its possessing medical properties which are not possessed by any other heretofore known tablet or lozenge base material and therefor by itself could be formed into tablets or lozenges possessing medical properties that are releasable in mouth fluids through sucking action.

Suckable, sugarfree, structurally sound and hard at room temperature, nonhygroscopic, noncariesforming, medically active tablets or lozenges possessing maximum stability and shelflife, prepared by the use of the new edible and palatable nonsugarbase, nonhygroscopic, cold water insoluble and structurally sound and hard at room temperature compounded tablet or lozenge base material possessing medical properties of its own of the invention, include such as mouth-refreshing; suckable tablets or Lozenges; cold and cough suckable tablets or lozenges; Mouth-treatment tablets or lozenges for the treatment of affections of the mouth and throat as of pyorrhea alveolaris, gum inflammations and the like; flavoring suckable tablets or lozenges; vitamin tablets or lozenges; anti-microbia suckable tablets or lozenges, and the like.

The other ingredients, incorporated in the new tablets or lozenges prepared by the use of the new nonsugarbase compounded tablet or lozenge base material possessing medical properties of its own of the invention, include such as generally used in the art of tablet or candy and lozenge making, for instance, suitable flavoring agents, mouth refreshing agents, artificial sweeteners, coloring matter, vitamins, drugs, antimicrobial agents, anti-inflammatory agents, anti-cough agents, anti-cold agents, pain relieving agents and the like. Mouth-refreshing suckable tablets or lozenges may contain peppermint oil, citric acid, cherry flavor extract, vanilla extract, raspberry extract, menthol, lemon extract and the like; cold and cough suckable tablets or lozenges may contain any of the generally used cold and cough agents, antibiotics, antimicrobials, pain-relieving agents and the like in addition to suitable desired flavoring, coloring and sweetening agents and possibly also vitamins; mouth treatment suckable tablets or lozenges may contain antiinflammatory agents, flavors, coloring matter, sweeteners, suitable drugs, vitamins and the like, although the use of tablets or lozenges prepared directly from the new nonsugarbase compounded tablet or lozenge base material of the invention provides already the necessary and desirable medical agent by itself to be useful in such mouth-treatment suckable tablets or lozenges and need merely the further addition of flavoring agents, sweeteners and, if desired, coloring matter; suckable flavoring tablets or lozenges may be used to replace sugar-based such tablets or lozenges and contain merely flavoring matter, coloring matter, sweeteners and the like; vitamin suckable tablets or lozenges may contain aside of the vitamin C provided by the new nonsugarbase compounded tablet or lozenge base material of the invention as result of its dissociation in mouth fluids, other vitamins that are available in the nonhygroscopic state, for instance the vitamin E in form of its dalpha-tocophery acid succinate as an effective anti-inflammatory agent, and vitamin A as acetate. Suckable tablets containing vitamin C alone or both vitamin C and E, derived through the use of the new nonsugarbase, compounded tablet or lozenge base material of the invention, also have the enormous advantage of being noncariesfor-ming when being sucked in the mouth fluids while exerting all the known actions of vitamin C, including its antimicrobial local effects, without attacking the tooth enamel. Anti-microbial suckable tablets or lozenges, prepared through the use of the new nonsugarbase compounded tablet or lozenge base material of the invention, may also contain other suitable antimicrobial agents such as a phenol with which the liberated l-ascorbic acid from the base material acts synergistically and reduces its toxicity without impeding thereby the antimicrobial effectiveness of said phenol, it being understood that, in addition, also other ingredients may be present in such tablets or lozenges, including flavors, sweeteners, coloring matter, pain-relieving agents and the like; too, it being understood that also other antimicrobial agents may be employed instead of a phenol, for instance quarternary ammonium compounds, antibiotics and the like and, it being also understood that more than one anti-bacterial agent may be employed for incorporation into tablets or lozenges prepared with the use of the new nonsugarbase compounded tablet or lozenge base material of the invention, for instance a quarternary ammonium compound and an aromatic alcohol such as benzyl alcohol.

My invention is based upon my discovery that the, hitherto thought of to be unsuitable as a tablet or lozenge base material solid higher fatty acid monoester of sorbitan sorbitan monostearate, which is a nonhygroscopic, cold-Water insoluble, structurally soft and Weak, edible and palatable material, can be rendered suitable for such use by the incorporation therein and compounding therewith suitable amounts of the edible and palatable, stable and nonhygroscopic, water soluble and structurally hardcrystallinic organic acid metal salt possessing medical properties calcium ascorbate dihydrate, such as described in US. Pats. 2,596,103 and 2,631,155 by Ruskin, 1952-53, either alone or in conjunction with a phosphate salt possessing anti-caries activity and capable of effectively acting as calcium mineral balancing agent metabolically and as partial replacement for said calcium ascorbate dihydrate itself, such as the almost water insoluble magnesium phosphate(di-basic), whereby the properties of both salts are transferred to the newly formed resulting compounded table or lozenge base material, including the properties of calcium ascorbate dehydrate which is quite well-tolerated by the gastrointestinal tract, exerts antiirritant properties, anti-inflammatory properties, antiscorbutic properties, beneficial circulatory properties and effects, beneficial effects in the treatment of affections of the mouth and throat including sinus infections, pyogenic inflammations of the nose and nasal accessory sinuses and in the treatment of gum inflammations such as pyorrhea alveolaris in which case calcium ascorbate acts antipyorrheally and anti-hemorrhageally and reduces the tendency of gums to bleed as Well as increases the firmness of blood vessel structures. In addition, also the property of calcium ascorbate to prevent caries formation in teeth by inhibiting the destructive attack on the tooth enamel by acids present and formed in the mouth is being transferred to the newly compounded tablet or lozenge base material of the invention, as well as also its well-known antihistaminic eiTect exerted bronchiologically and its anti-allergic effects so well known and recorded in literature and, most importantly, the anti-microbial eflects of its l-ascorbic acid liberated from the compound salt calcium ascrobate as it dissociates during sucking action in mouth fluids. Furthermore, the new nonsugarbase compounded tablet or lozenge base material thus prepared possesses the additional anti-carious property of the partial substituent for the calcium ascorbate, where used, as

well as its calcium mineral balancing property, which it metabolically utilizes in tablets or lozenges prepared thus by the very use of the nonsugarbase compounded tablet or lozenge base material of the invention containing both calcium ascorbate dihydrate and dibasic magnesium phosphate. However, the most important factor is that the new base material as prepared from the soft and structurally weak solid higher fatty acid monoester of sorbitan sorbitan monostearate by the incorporation and compounding therein of suitable amounts of the said calcium ascorbate dihydrate, alone or in conjunction with its partial replacement by dibasic magnesium phosphate, results in the formation of an edible and palatable, stable and nonhygroscopic, water insoluble and structurally sound and hard at room temperature, nonsugarbase, compounded tablet or lozenge material possessing medical properties of its own which can be used for the production of sugarfree, suckable, structurally sound and hard at room temperature, nonhygroscopic, noncariesforming tablets or lozenges possessing maximum stability and shelflife and dispersible and or dissolvable in mouth fluids by sucking action for the release of its properties, including the medical properties of the said nonsugarbase compounded tablet or lozenge base material used in the preparation of said tablets or lozenges.

It is also new that a nonhygroscopic and water insoluble material should become useful as a tablet or lozenge base material as usually such nonhygroscopic and water insoluble materials are not dispersi'ble and/or dissolvable in mouth fluids through any kind of sucking action. However, it has been discovered that the water insoluble and nonhygroscopic sorbitan mono-stearate could be brought into dispersion and/or dissolution in mouth fluids by the very presence of nonhygroscopic calcium ascorbate dihydrate, provided suflicient amounts are added thereto. Obviously, the ready dissociability of the calcium ascorbate dihydrate in mouth fluids and body fluids, which has been documented in the literature, causes the formation of a calcium soap with the said sorbitan monostearate and, as result thereof, dispersion and/or dissolution of the whole compounded tablet or lozenge base material of the invention in mouth fluids by way of sucking action, and thereby renders the hitherto thought of unsuitable sorbitan monostearate suitable for use as tablet or lozenge base material, respectively part of a composition representing a tablet or lozenge base material, which, in addition, also possesses medical properties by virtue of same being possessed by the calcium ascorbate dihydrate.

The resulting new base material characterizes itself by possessing an unexpected homogeneous texture heretofore thought impossible to achieve with a material like calcium ascorbate dihydrate, which is hard-crystallinic and gritty, provided the proper amounts of the latter have been incorporated in the sorbitan monostearate and proper means have been employed to do this. Grittiness and as caries-protective agent as which phosphates have proven effectiveness well documented in the literature, and all these additional beneficial effects of the partial substitution of calcium ascorbate dihydrate by the dibasic magnesium phosphate are obtained without thereby reducing but rather improving the dispersibility and/or solvability of tablets or lozenges prepared by the use of such a new tablet or lozenge base material containing both calcium ascorbate dihydrate and dibasic magnesium phosphate. The employment of the calcium ascorbate d'ihydrate with dibasic magnesium phosphate in the composition of the new tablet or lozenge base material of the invention is also essential because the use of dibasic magnesium phosphate alone, or in concentrations beyond certain limits, would not result in suitable tablet or lozenge base materials as they would be of too soft a structure and also fail to properly disperse and/ or dissolve in mouth fluids by sucking action, since, by itself, the dibasic magnesium phosphate is a soft and almost water-insoluble material and it had been found that it was the action of calcium ascorbate dihydrate which had caused the solvation of the almost water-insoluble dibasic magnesium phosphate in analogy to the well documented solubilizing effects of Water soluble salts of organic oxyacids (see: Neuberg et al., Zeitschrift f. Vitamin, Hormon-Fermentforschung, February 1949, pages 480-492, particularly page 486), eifecting a co-dispersing and/or co-dissolving action upon dibasic magnesium phosphate.

It was found that in order to procure a suitable compounded tablet or lozenge base material useful for the purposes of the invention, certain definite weight proportions between the sorbitan monostearate and calcium ascorbate dihydrate components must be maintained in order to obtain the desired homogeneous texture in the finally resulting material and to overcome the unpleasant taste of calcium ascorbate dihydrate itself which otherwise would act as a deterrent to its use by the public. Thus, by weight percentages, satisfactory tablet or lozenge base materials are produced when the weight percentage ratios between the sorbitan monostearate and the calcium ascorbate dihydrate are maintained between 38 to 50 parts by weight and from 60 to 30 parts by weight, with the inbetween weight percentages to be supplied by other desirable and suitable component ingredients to be added to the to be prepared tablet or lozenge mass, including amounts assignable to any if used dibasic magnesium phosphate.

Examples of suitable formulations suggested for the preparation of compounded tablet or lozenge base materials of the invention are presented in the following table, in which the amount of other suitable component ingredients other than the dibasic magnesium phosphate is arbitrarily set at 2 weight percentages, including such agents as flavoring agents, mouth refreshing agents, artificial sweeteners, coloring matter, vitamins, drugs, anti-micro bial agents, anti-inflammatory agents, anti-cough agents, anti-cold agents, pain relieving agents, and the like.

TAB LE-FO RMULATIO NS Ingredients (in parts by weight percentages) 1 3 4 5 6 7 8 9 l l1 l2 13 14 l 16 17 18 19 20 sorbitan monostearate 43 50 43 40 38 46 43 45 44 40 45 40 46 50 47 Calcium ascorbate dihydrate 41 48 51 38 41 41 53 38 34 38 33 Magnesium phosphate, (ll-has 14 18 15 10 9 16 10 12 13 5 l5 8 18 10 18 (J ther ingredients 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 2 in suckable tablets or lozenges would, of course, have made any usefulness of a tablet or lozenge base material illusory as the unpleasant sensation of grittiness in the mouth would make tablets or lozenges nonsalable.

The use of dibasic magnesium phosphate as a partial substituent for the calcium ascorbate dihydrate, used in the preparation of the new base material of the invention, acts not only as calcium mineral balancing agent which is metabolically utilized as the dissolved fractions of the material are swallowed, but also as cost reduction agent Experiments have also shown that the limiting amounts of dibasic magnesium phosphate addable to the composition of the new tablet or lozenge base material of the invention, without affecting the prime requisites such as nonhygroscopicity, structural soundness and hardness at room temperature, dispersibility and/or dissolubility in mouth fluids through sucking action, homogeneous texture, edibility and palatibility as well as shelflife and stability of tablets or lozenges prepared therewith, are 18 weight percentages. Experiments have also shown that sorbitan for calcium ascorbate dehydrate, which is very expensive, monostearate could not be replaced as one of the basic component raw materials for the preparation of the new tablet or lozenge base material of the invention, for instance, by the use of sorbitan mono-palmitate because this latter material is not only not nonhygroscopic but also not water insoluble and not accepted by the Food and Drug Administration for use in foods. Tests have shown that tablet or lozenge base materials made by the use of sorbitan mono-palmitate possessed but a very low stability and short shelflife. Thus the use of the sorbitan monostearate is specific and essential for the successful creation of a more suitable nonsugarbase tablet or lozenge base material than has ever been produced heretofore, it naturally being of the essence that all of the basic components forming the said new compounded tablet or lozenge base material of the invention had to be nonhygroscopic, non-toxic, edible, stable, sugarfree and noncariesforming in nature. This made it impossible to employ any other kind of calcium ascorbate than the dihydrate compound as all its other forms are hygroscopic. This material was found to be irreplaceable also on account of its hard crystallinity which so beneficially conferred to the new tablet or lozenge base material of the invention the required hardness and structural soundness at room temperature as well as medical properties not possesed by any other tablet or lozenge base material, although a search for another material to serve as substitute for said calcium ascorbate dihydrate revealed the existence of the organic calcium salt calcium acid lactate dihydrate, also called acid calcium lactate, of Wulfing and Bosch (British Pat. 229,192 of 1925) which is also nonhygroscopic but lacks the hard crystallinity of calcium ascorbate dihydrate and is unable to form with sorbitan monostearate a structurally hard and sound at room temperature material and is neither capable of dissociation in mouth fluids through sucking action to enable its calcium ions to form with the sorbitan monostearate dispersible and/ or dissolvable substances.

Thus, as calcium ascorbate dihydrate may be the only suitable substance for the purposes of this invention, it may be used as is or as a 1% methocel coated material, both available in commerce. Both materials are extremely stable materials and can be processed without harm thereto even under heating conditions, for instance also in the presence of open air access during such heating and test have shown that for instance both materials will withstand 250 F. heat exposure for periods up to 17 minutes in a current of open air without detriment to structure and l-ascorbic acid potency. Such tests have shown that 99.63%, respectively 100% potencies as regards l-ascorbic acid potency were retained in non-coated, respectively coated calcium ascorbate dihydrates that had been exposed in an electric oven to 250 F. for 17 min. time in a current of air, establishing beyond any possible doublt the usefulness of the calcium ascorbate dihydrate for the purposes of this invention, as shown in the following, heat of this range is needed in the compounding of the new tablet or lozenge base material of this invention. However, how stable the calcium ascorbate dihydrate actually is had previously also been documented by Ruskin and Merrel (Science, 1947, v. 105, pp. 504-5), who found that after 6 hours exposure to boiling toluene, which boils at 240.8 F., only a slight decomposition took place. The results of these tests, although not being properly comparable, would however indicate that calcium ascorbate dihydrate is stable enough to be processed in the presence of air at temperatures up to 250 F. for periods of time not exceeding 17 minutes, without sulfering structural or ascorbic acid potency damages. Until this discovery of the heat stability of the calcium ascorbate dihydrate, it was not though to be practical to use any salt or ascorbic acid in processing requiring high temperature exposure for any length of time as such exposure was generally considered detrimental to the potency of l-ascorbic acid possessed by any such salt and I believe that I am the first to exploit this newly discovered property of calcium ascorbate dihydrate in the preparation of my new tablet or lozenge base material of the invention which is useful for the production of improved suckable, sugarfree, medically active tablets or lozenges possessing maximum stability and shelflife.

In carrying out the invention and preparing the tablet or lozenge base material of the invention, by suggested compositions of formulations suitably producible, without limiting the invention thereto, as they appear in the table, the following method examples are given:

METHOD EXAMPLE 1 After weighing the components of the formulations separtely, sorbitan monostearate, component one, is placed in a suitable receptacle equipped with means for heating, stirring and kneading, and heated therein until a clear molten state is reached. The temperature is then about 250 F. and further heat is then withdrawn from the receptacle. During the heating and melting of the sorbitan mono stearate, simultaneously, the calcium ascorbate dihydrate and dibasic magnesium phosphate where used in admixture are being preheated by suitable means, for instance, in a separate receptable, to an appropriate temperature comparable with the temperature used to obtain a clear melt of sorbitan monosterate, for instance, between 230-240 F., to facilitate easier compounding of the same with the sorbitan monosterate.

At this point, the preheated calcium ascorbate dihydrate and, where used also the dibasic magnesium phosphate, is or are added to the molten sorbitan monostearate and incorporated therein and compounded therewith by the operation of the stirring, mixing and kneading means with which the receptacle is equipped. This is followed by further homogenization in suitable homogenization equipment, for instance such as is widely known and used in the art employing needle valves through which the material is squeezed under pressure and extruded, to cause the formation of a highly densified strang of the new compounded tablet or lozenge base material which, after cooling to room temperature, is structurally sound and hard and of homogeneous texture and possesses medical properties of its own and can be softened for the incorporation of other desired ingredients for use in tablets or lozenges and re-homogenized and extruded or cast and shaped into desirable forms as tablets or lozenges ready to be sold. This may be accomplished through the use of traditional candy making machinery such as known in the art.

The finished base material represents a nonsugarbase, edible, palatable, suckable, nonhydroscopic, structurally sound and hard at room temperature, noncariesforming material which possesses medical properties of its own, which can 'be used for the production, by incorporating therein other ingredients desired for such purpose, of suckable, sugarfree, structurally sound and hard at room temperature, nonhydroscopic, noncariesforming tablets or lozenges possessing not only the medical or other properties as desired but also the medical properties of the base material all of which being releasable through sucking action in mouth fluids and possessing maximum stabilities and shelflifes by virtue of nonhygroscopicity conferred to the same by the said new base material.

METHOD EXAMPLE 2 After weighing the components of the desired formulations separately, namely the sorbitan monosterate, calcium ascorbate dihydrate and, Where used, the dibasic magnesium phosphate, all being provided in powder or crystal form, same are mixed together thoroughly and then introduced into a suitable means equipped with heating means, kneading and homogenizing devices and heated therein under kneading and homogenizing action until a temperature of 250 F. is reached, after which further heating is discontinued and the mass pressed through the needle valve of the homogenizing end of the treatment receptacle and extruded therefrom in form of a homogeneously textured mass which is the finished new compounded tablet or lozenge base material of the invention which, after cooling down to room temperature, is a structurally sound and hard mass possessing medical properties of its own and softenable by heating for the further incorporation therein of other ingredients desired to be present in the tablets or lozenges to be prepared therewith, followed by rehomogenization and further working up to shapes and forms desired as tablets or lozenges in generally known standard candy making machines.

The base material obtained in accordance of either method 1 or method 2 when used for the preparation of tablets or lozenges by incorporating therein other desired ingredients may after such incorporation not only be made into such individual tablets or lozenges by the use of standard candy making machinery but also, if desired, by way of casting into molds which are left to be chilled or pressing into forms to be left to be chilled or any other appropriate means and without limiting the invention thereto. In addition, the formation of tablets or lozenges through the use of the new compounded tablet or lozenge base material may take place also in one single step, whereby the compounded material is formed simultane ously as tablets or lozenges are formed therefrom, namely by the incorporation into the compounded mass of all the desired suitable ingredients for such tablets or lozenges before the said compounded material mass is finished and while being in the process of kneading and homogenizing. This is exemplified in method Example 3.

METHOD EXAMPLE 3 Sugarfree, cariespreventive, suckable tablets or lozenges are directly prepared by using either method 1 or method 2 means of preparing the compounded base material and adding thereto for incorporation any of the desired other ingredients of to be prepared tablets or lozenges, including flavoring agents, artificial sweetners, coloring matter, vitamins, antimicrobials, pain-relieving agents, mouth refreshng agents, drugs, anti-cough and anti-cold agents and the like, depending on the type of tablet or lozenges to be prepared, and thereafter mixing, kneading and homogenizing the tablet or lozenge material thereby obtained and further working the same into individual tablets or lozenges through the use of conventional methods including standard candy making machinery and the like.

The resulting tablets or lozenges are ready for sale. Due to the absence of hygroscopicity in the new tablets or lozenges thus prepared, same do not require special wrappings or coatings and possess maximum stability and shelflife.

Examples of some of the tablets or lozenges prepared in accordance with the invention, without limiting the invention thereto, are:

Examples of Tablets or Lozenges new sugarfree, suckable, structurally sound and hard at room temperature, nonhygroscopic, non-cariesforming and medicated tablets or lozenges prepared by the employment of the new nonsugarbase compounded tablets or lozenge base material of the invention possessing medical properties of its own, include such as:

(1) Month refreshing tablets or lozenges, containing illustratively but not limited thereto the following ingredients:

' Formulas Ingredients in percentages by weight A B C D E Base material of the invention. 98.00 98.00 98.00 98.00 95.00 Acetylselicylic acid or salt ofit 3.00 Benzocaine Saccharim- Menthol Eucalyptol. Phenol. Thymol .t Cetylpyr'idium chloride Cetyltrimethylammonium bromide 0.05 0. 02 Antibiotic(tetracycline, as

example 0. 30 Vitamin A, solid form, as

powder 0. 10 0. 10 Vitamin E, as dalphatoce pheryl acid succinate 0.10 0.60 0.45 0. 45 Flavoring, such as peppermint oil 0.65 Flavoring, such as cherry extract 0.18 Flavoring, such as raspberry extract 0.78 Flavoring, such as lemon flavoring .-u 0.28 Coloring matter 0. 02 0. 02 0. 02 0. 02 0. 02 Citronellal (stereoiscmeric aldehyde) 0. 38 Benzyl alcohol 0.30 0.30

As indicated in the Formulas (2)E and (3)E, the percentage weight of other ingredients is not limited to 2% as indicated in the formulation table pertaining to the tablet or lozenge base material compositions range, and such differences shall not be construed to limit the scope of the invention. However, where the amount of other ingredients to be incorporated into tablets or lozenges is more than 2%, the excess shall not reduce the amount of drbasic magnesium phosphate in formulations where used to below the fixed 2% in any of the formulations that may be used and shall in such cases rather reduce the amounts of calcium ascorbate dihydrate in the said basic material formulations.

(3) Mouth treatment or lozenges for the treatment of afiecttons of the mouth and throat as of pyorrhea: alveolarzs, gum inflammations and the like, containing illustratively but not limited thereto the following ingredients:

Formulas Ingredlents in percentages by weight A B C D E Base material of the invention 98.00 98.00 98.00 98.00 95.00 Saccharrn- 0. l5 0. 15 0. l2 0. l2 0. 10 Peppermint 011-- 0.50 0.20 0. 49 0.75 Coloring matter 0.02 0. 02 0. 02 0. 02 0. 02 dAlpha tocopheryl acid suecrnate 1.00 1.25 1.00 3.00 Benzocame- 0.02 0.02 0. 02 0. 02 Eucalyptol 0.26 0. 02 0.34 0.10 Vitamin A, solid, as powder 0.30 0.13 Gum of myrrh 0.05 0.04 Cherry flavoring 0.50 0.50 0.25 Acetylsalicylic acid or salt oilt- 0. 25 1. 00

(4) Flavoring tablets or lozenges, containing illustratively but not limited thereto the following ingredients:

Formulas Ingredients in percentages by weight A B G D E Formulas Ingredients in percentages Base material of the invention.. 98. 00 98. 00 98. 0O 98. 00 98. 00 by Weight A B O D E Menthol 0. 33 0. 60 0. 43 0. 15 Saccharin- 0. 15 0. 14 0. 15 0. 15 Base material of the invention.. 98. 0O Peppermint oil 1. 00 O. 50 Saceharm. 0.15 Edible coloring matter 0. 02 0. 02 0. 02 0. 02 0. 02 Sodium or calcium cyclamate," 0. 10 Dalphetocopheryl acid Lemon flavoring 1. 50

succinate 0. 50 0. 50 Mint flavoring Chlorophyll Chocolate powder for flavoring. Raspberry flavoring. Cherry flavoring Lemon flavoring. Strawberry flavoring Cherry flavoring- Coloring matter- Vanillin Vanillin Sodium or calcium cyclamate Menthol 1 1 (5) Vitamin tablets or lozenges, containing illustratively but not limited thereto the following ingredients:

The amounts of vitamins releasable from these preparations are: In Formula (5)A 1512.5 I.U. vitamin E and from 26,812 mgs. vitamin C to 48,750 mgs. vitamin C activities per 100 grams tablet or lozenge, depending on which base formula from the table is selected. The amounts of vitamins releasable from Formula (5)B are 1500.4 I.U. vitamin E and from 26,812 to 48,750 mgs. vitamin C activities, depending on which base formula is selected and, in addition, also 29,040 LU. vitamin A activity if the vitamin A used is the vitamin A-acetate. The amounts releasable from Formula (5)C are 1210 LU. of vitamin E and from 26,812 to 48,750 mgs. vitamin C activities depending on which base formula from the table is selected. The amounts of vitamins releasable from Formula (5)D are 1815 LU. vitamin E and from 26,812 to 48,750 mgs. vitamin C, depending on which base formula from the table is selected and, finally, the amounts of vitamins releasable from the Formula (5)E are 4,416.5 LU. Vitamin E, from 26,812 to 48,750 mgs. vitamin C, depending on which base formula from the table is selected and 580,000 LU. Vitamin A as the vitamin A-acetate, all per 100 grams of finished tablet or lozenge.

(6) Anti-microbial suckable tablets or lozeng s, containing illustratively but not limited thereto the following ingredients:

Formulas Ingredients in percentages by weight A B C D E Base material of the invention 98. 00 Flavoring agents, any desirable- Artificial sweetener saecharin ym Cetyl pyridium chl Cetyl trimethylammonium bromide 0. 05 Tetracycline dihydrate 1. 00

As a suitable flavoring agent may be used essential oils, such as peppermint oil, oil of clove, vanillin, cherry flavor oil, citronellol and the like, all of which possess antibacterial properties of its own. It should be pointed out, as already mentioned before, that the synergism between 1- ascorbic acid released from its union with calcium in calcium ascorbate dihydrate and phenolic compounds will tend to allow phenols to exert anti-microbial activities without exerting toxicities and since l-ascorbic acid itself acts antimicrobial, tablets and lozenges prepared with both exert obviously a more antimicrobial action than either group alone without addition of the other.

It should be pointed out that all the given formulations are merely examples of tablets or lozenges that can be prepared by the use of the base material of this invention and shall be deemed merely illustrative and not restrictive. In the appended claims the term tablets shall be deemed also to stand for lozenges and the use of the term dissolvable shall be deemed also to stand for dispersible.

I claim:

1. Nonsugarbase, nonhygroscopic, tablet base material for use in the preparation of suckable, noncaries forming tablets, comprising sorbitan monostearate compounded with calcium ascorbate dihydrate; the percentage weights of the sorbitan monostearate being from 38 to 50, and of the calcium ascorbate dihydrate from 60 to 30.

2. Nonsurgarbase, nonhygroscopic, tablet base material for use in the preparation of suckable, noncaries forming tablets, comprising sorbitan monostearate compounded with calcium ascorbate dihydrate and dibasic magnesium phosphate; the percentage weights of the sorbitan monostearate being from 39 to 50, of the calcium ascorbate dihydrate being from 57 to 30, and of the dibasic magnesium phosphate being from 2 to 18.

References Cited Chemical Abstracts (I): vol: 53, entry 22513f, 1959. Chemical Abstracts (II): vol. 61, entry 7600d, 1964.

RICHARD L. HUFF, Primary Examiner UNITED STATES PATENT OFFICE CERTIFICATE OF CORRECTION Patent No 3,525 791 August 25 1970 Gerhard W. Ahrens It is certified that error appears in the above identified patent and that said Letters Patent are hereby corrected as shown below:

In the heading to the printed specification, line 9, "New York, N. Y." should read Brooklyn, N. Y. Column 2, line 41, "protection" should read production line 44, after "gained" insert a comma. Column 3, line 75, "tocophery" should read tocopheryl Column 4, line 49, "table" should read tablet line 71, "ascrobate" should read ascorbate line 30, "the," should read the Column 7, line 52, "doublt" should read doubt line 68, Jthough" should read thought Column 8, lines 12 and 13, separtly" should read separately Column 9, line 53, "Examples of Tablets or Lozenges new sugarfree" should read Examples of Tablets or Lozenges as a heading; and New sugarfree as the beginning of the paragraph on line 11,

same column 9.

Signed and sealed this 23rd day of March 1971.

(SEAL) Attest:

EDWARD M.PLETCHER,JR. WILLIAM E SCHUYLER, JR. Attesting Officer Commissioner of Patents 

